Development and Evaluation of Avanafil Self-nanoemulsifying Drug Delivery System with Rapid Onset of Action and Enhanced Bioavailability

Abstract

Utilization of lipid-based drug delivery systems has recently gained focus for drugs characterized by poor aqueous solubility. The improved aqueous solubility overcomes one of the main barriers that limit their bioavailability. The objective of this work was to improve the solubility and oral bioavailability of Avanafil (AVA), a recently approved second generation type 5 phospodiesterase inhibitor used for erectile dysfunction.AVA was formulated as self-nanoemulsifying drug delivery system (SNEDDS) utilizing various oils, surfactants, and cosurfactants. The solubility of AVA in various oils, surfactants, and cosurfactants was determined. Ternary phase diagram was constructed to identify stable nanoemulsion region. The prepared AVA loaded SNEDDS were assessed for optical clarity, droplet size, conductivity, and stability studies. In vitro drug release and in vivo pharmacokinetic parameters using animal model were also investigated. Results revealed that stable AVA (SNEDDS) were successfully developed with a droplet size range of 65 to 190 nm. SNEDDS composed of 25% dill oil, 55% Tween 80, and 20% propylene glycol successfully improved solubilization of AVA (over 80% within 30 min) vis-a-vis the powder AVA (35% within 30 min). In vivo pharmacokinetic showed a significant (P < 0.05) increase in Cmax, reduction in Tmax, and SNEDDS enhanced the bioavailability in the rats by 1.4-fold when compared with pure drug.

RETRACTED: Attenuation of Benign Prostatic Hyperplasia by Optimized Tadalafil Loaded Pumpkin Seed Oil-Based Self Nanoemulsion: In Vitro and In Vivo Evaluation

“…upper limit), takes place. Besides enhancing stability, these lipid-based nano-entities employed as novel drug delivery systems (DDSs) are indicated to improve drug solubility, dissolution behavior in the GIT, and thus are known to increase the absorption of the poorly water-soluble drugs [28][29][30][31][32].…”

“…Similar results obtained in vivo would indicate the significance of this compound as a supportive treatment for conditions, such as BPH, which frequently occurs in males aged 50 and over [25][26][27].Self nano-emulsified drug delivery systems (SNEDDSs) are increasingly being utilized in the pharmaceutical field as a vehicle or drug delivery system in various formulations, such as creams, foams, liquids, and sprays. This is because of their high degree of drug permeation through tissues, stability, and fewer side effects compared to other modern drug delivery systems [28][29][30][31][32]. SNEDDSs are superior to microemulsion because of their smaller size, larger surface area, and absence of any inherent creaming, flocculation, coalescence, or sedimentation.…”

Formulasi Sediaan Nano Herbal Tempuyung (Sonchus arvensis L.) dalam Bentuk Self Nano-Emulsifying Drug Delivery System (SNEDDS)

“…SNEDDS telah banyak dikembangkan untuk meningkatkan kelarutan dan ketersediaan hayati dari berbagai obat yang lipofil diantaranya glipizida [8], avanafil [9], evafirenz [10] dan glimepirida [11]. …”

Avanafil Liposomes as Transdermal Drug Delivery for Erectile Dysfunction Treatment: Preparation, Characterization, and <i>In vitro, Ex vivo </i>and <i>In vivo</i> Studies

“…Avanafil is a phosphodiesterase-5 enzyme inhibitor and a second-generation erectile dysfunction medication [2,3]. Avanafil has advantages over other PDE5 inhibitors, as it is more selective for the PDE5 isoenzyme and a variety of cellular targets than sildenafil and tadalafil [4].…”

“…Therefore, the enhancement of its bioavailability is essential for the development of effective clinical formulations [4].…”